Z-WEHD-FMK
Treatment of infected cells with pan-caspase inhibitor IV and Z-WEHD-FMK, an inhibitor of inflammatory caspases, elicited a near-complete blockage of C. trachomatis-induced cleavage of golgin-84. Golgin-84 cleavage was blocked via treatment of infected cells with Z-WEHD-FMK, resulting in a lack of Golgi fragmentation and a 2-log reduction in numbers of infectious bacteria.
We treated infected cells with Z-WEHD-FMK, effectively preventing Golgi fragmentation, or with DMSO as a control and then labelled cells with fluorescent ceramide. Confocal images revealed that ceramide was rapidly incorporated into the inclusion membrane within DMSO-treated cells and accumulated inside the inclusion in bacterial membranes. In contrast, Z-WEHD-FMK-treated cells were only slightly fluorescent as the majority of lipid accumulated in a Golgi-like structure outside the inclusion1.
General caspase inhibitor (Z-Asp-CHz-DCB) and capase-5 inhibitor (Z-WEHD-FMK) could not induce rRNA fragmentation treated with ECyd. Caspase-5 (ICErei Ill/TY), member of ICE protease, activated pathway may be concerned with ECyd induced rRNA fragmentation2.
References:
1. D. Heuer, A.R. Lipinski et al. Chlamydia causes fragmentation of the Golgi compartment to ensure reproduction. NATURE, 457, 2009
2. Kamada, S., Funahashi, Y. and Tsujimoto, Y.(1997) Cell Death Diff. 4, 473-478.
- 1. Yan-Yan Heng, Hui-Juan Shang, et al. "Sodium tanshinone IIA sulfonate ameliorates neointima by protecting endothelial progenitor cells in diabetic mice." BMC Cardiovasc Disord. 2023 Sep 11;23(1):446. PMID: 37697234
- 2. Shouwen Chen, Peng Jin, et al. "Dual function of a turbot inflammatory caspase in mediating both canonical and non-canonical inflammasome activation." Dev Comp Immunol. 2021 Aug;121:104078. PMID:33794278
- 3. WeiWei, Xiao-XueLi, et al. "Inhibition of vascular neointima hyperplasia by FGF21 associated with FGFR1/Syk/NLRP3 inflammasome pathway in diabetic mice." Atherosclerosis. Available online 29 August 2019.
- 4. Yang D, Zheng X, et al. "Sensing of cytosolic LPS through caspy2 pyrin domain mediates noncanonical inflammasome activation in zebrafish." Nat Commun. 2018 Aug 3;9(1):3052. PMID:30076291
| Storage | Store at -20°C |
| M.Wt | 763.77 |
| Cas No. | 210345-00-9 |
| Formula | C37H42FN7O10 |
| Synonyms | Z-Trp-Glu(OMe)-His-Asp(OMe)-FMK |
| Solubility | insoluble in H2O; ≥26.32 mg/mL in EtOH with ultrasonic; ≥46.33 mg/mL in DMSO |
| Chemical Name | methyl (4S)-5-[[(2S)-1-[[(3S)-5-fluoro-1-methoxy-1,4-dioxopentan-3-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-[[(2S)-3-(1H-indol-3-yl)-2-(phenylmethoxycarbonylamino)propanoyl]amino]-5-oxopentanoate |
| SDF | Download SDF |
| Canonical SMILES | COC(=O)CCC(C(=O)NC(CC1=CN=CN1)C(=O)NC(CC(=O)OC)C(=O)CF)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)OCC4=CC=CC=C4 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Chlamydia trachomatis (C. trachomatis)-infected HeLa cells |
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Reaction Conditions |
80 μM Z-WEHD-FMK for 9 h incubation |
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Applications |
Z-WEHD-FMK (80 μM; 9 h) elicited a near-complete blockage of C. trachomatis-induced cleavage of golgin-84 and increased GM130 expression in cells. Z-WEHD-FMK treatment resulted in a 2-log reduction in numbers of infectious bacteria, which could be reversed by knocking down golgin-84. Thus, Z-WEHD-FMK could effectively prevent Golgi fragmentation, and was used to explore the role of fragmentation of the Golgi compartment in Chlamydia reproduction. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Heuer D, Rejman Lipinski A, Machuy N, et al. Chlamydia causes fragmentation of the Golgi compartment to ensure reproduction. Nature, 2009, 457(7230): 731-735. |
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| A synthetic peptide that irreversibly inhibits caspase-5 and related caspase activity. | ||||||
| Targets | caspase-5 | |||||
| IC50 | ||||||
Quality Control & MSDS
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